3o0u

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<StructureSection load='3o0u' size='340' side='right'caption='[[3o0u]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
<StructureSection load='3o0u' size='340' side='right'caption='[[3o0u]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[3o0u]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3O0U OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3O0U FirstGlance]. <br>
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<table><tr><td colspan='2'>[[3o0u]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3O0U OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3O0U FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=O47:3-{2-[(E)-IMINOMETHYL]-6-PROPYLPYRIMIDIN-4-YL}-N,N-DIMETHYL-5-(TRIFLUOROMETHYL)BENZAMIDE'>O47</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.8&#8491;</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">CTSK, CTSO, CTSO2 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=O47:3-{2-[(E)-IMINOMETHYL]-6-PROPYLPYRIMIDIN-4-YL}-N,N-DIMETHYL-5-(TRIFLUOROMETHYL)BENZAMIDE'>O47</scene></td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Cathepsin_K Cathepsin K], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.38 3.4.22.38] </span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3o0u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3o0u OCA], [https://pdbe.org/3o0u PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3o0u RCSB], [https://www.ebi.ac.uk/pdbsum/3o0u PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3o0u ProSAT]</span></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3o0u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3o0u OCA], [https://pdbe.org/3o0u PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3o0u RCSB], [https://www.ebi.ac.uk/pdbsum/3o0u PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3o0u ProSAT]</span></td></tr>
</table>
</table>
== Disease ==
== Disease ==
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[[https://www.uniprot.org/uniprot/CATK_HUMAN CATK_HUMAN]] Defects in CTSK are the cause of pycnodysostosis (PKND) [MIM:[https://omim.org/entry/265800 265800]]. PKND is an autosomal recessive osteochondrodysplasia characterized by osteosclerosis and short stature.<ref>PMID:8703060</ref> <ref>PMID:9529353</ref> <ref>PMID:10491211</ref> <ref>PMID:10878663</ref>
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[https://www.uniprot.org/uniprot/CATK_HUMAN CATK_HUMAN] Defects in CTSK are the cause of pycnodysostosis (PKND) [MIM:[https://omim.org/entry/265800 265800]. PKND is an autosomal recessive osteochondrodysplasia characterized by osteosclerosis and short stature.<ref>PMID:8703060</ref> <ref>PMID:9529353</ref> <ref>PMID:10491211</ref> <ref>PMID:10878663</ref>
== Function ==
== Function ==
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[[https://www.uniprot.org/uniprot/CATK_HUMAN CATK_HUMAN]] Closely involved in osteoclastic bone resorption and may participate partially in the disorder of bone remodeling. Displays potent endoprotease activity against fibrinogen at acid pH. May play an important role in extracellular matrix degradation.
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[https://www.uniprot.org/uniprot/CATK_HUMAN CATK_HUMAN] Closely involved in osteoclastic bone resorption and may participate partially in the disorder of bone remodeling. Displays potent endoprotease activity against fibrinogen at acid pH. May play an important role in extracellular matrix degradation.
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Cathepsin K]]
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[[Category: Homo sapiens]]
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[[Category: Human]]
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[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Fradera, X]]
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[[Category: Fradera X]]
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[[Category: Uitdehaag, J C.M]]
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[[Category: Uitdehaag JCM]]
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[[Category: Zeeland, M van]]
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[[Category: Van Zeeland M]]
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[[Category: Bone]]
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[[Category: Covalent 2-cyano-pyrimidine inhibitor]]
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[[Category: Hydrolase]]
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[[Category: Hydrolase-hydrolase inhibitor complex]]
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[[Category: Reversible covalent bond between cys25 and ligand]]
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Current revision

Cathepsin K covalently bound to a cyano-pyrimidine inhibitor with improved selectivity over hERG

PDB ID 3o0u

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